Advances in Mycobacterial Isocitrate Lyase Targeting and Inhibitors

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F12%3A10127171" target="_blank" >RIV/00216208:11160/12:10127171 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.ingentaconnect.com/content/ben/cmc/2012/00000019/00000036/art00005" target="_blank" >http://www.ingentaconnect.com/content/ben/cmc/2012/00000019/00000036/art00005</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.2174/092986712804485782" target="_blank" >10.2174/092986712804485782</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Advances in Mycobacterial Isocitrate Lyase Targeting and Inhibitors

Popis výsledku v původním jazyce

Isocitrate lyase plays a key role for survival of Mycobacterium tuberculosis in the latent form during a chronic stage of infection. This enzyme is important for M. tuberculosis during steady stage growth when it converts isocitrate to succinate and glyoxylate. Then, the glyoxylate is condensed with acetyl-CoA to form malate by malate synthase. The carbon conserving glyoxylate pathway has not been observed in mammals; therefore, it has been determined as a potential drug target for discovery of a new antituberculosis agent. Novel active molecules should shorten the duration of therapy, prevent resistance development and eliminate latent disease. The review summarizes recent progresses in isocitrate lyase inhibitors, overviews structural analogues of several metabolic intermediates (3-nitropropionate, 3-bromopyruvate, itaconate, itaconic anhydride), peptide inhibitors, and recently developed inhibitors with various chemical structures. The largest inhibitory activity against isocitrate

Název v anglickém jazyce

Advances in Mycobacterial Isocitrate Lyase Targeting and Inhibitors

Popis výsledku anglicky

Isocitrate lyase plays a key role for survival of Mycobacterium tuberculosis in the latent form during a chronic stage of infection. This enzyme is important for M. tuberculosis during steady stage growth when it converts isocitrate to succinate and glyoxylate. Then, the glyoxylate is condensed with acetyl-CoA to form malate by malate synthase. The carbon conserving glyoxylate pathway has not been observed in mammals; therefore, it has been determined as a potential drug target for discovery of a new antituberculosis agent. Novel active molecules should shorten the duration of therapy, prevent resistance development and eliminate latent disease. The review summarizes recent progresses in isocitrate lyase inhibitors, overviews structural analogues of several metabolic intermediates (3-nitropropionate, 3-bromopyruvate, itaconate, itaconic anhydride), peptide inhibitors, and recently developed inhibitors with various chemical structures. The largest inhibitory activity against isocitrate

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

—

Projekt

<a href="/cs/project/NT13346" target="_blank" >NT13346: Design a enzymové cílení nových antibakteriálně účinných sloučenin vůči multilékově rezistentním kmenům</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2012

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Current Medicinal Chemistry

ISSN

0929-8673

e-ISSN

—

Svazek periodika

19

Číslo periodika v rámci svazku

36

Stát vydavatele periodika

NL - Nizozemsko

Počet stran výsledku

12

Strana od-do

6126-6137

Kód UT WoS článku

000311959800005

EID výsledku v databázi Scopus

—